A Novel Isoquinoline Derivative Anticancer Agent and Its Targeted Delivery to Tumor Cells Using Transferrin-Conjugated Liposomes |
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| Authors: | Xuewei Yang Shuang Yang Hongyu Chai Zhaogang Yang Robert J Lee Weiwei Liao Lesheng Teng |
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| Institution: | 1. College of Life Sciences, Jilin University, Changchun, China.; 2. College of Pharmacy, The Ohio State University, Columbus, United States of America.; 3. Department of Organic Chemistry, College of Chemistry, Jilin University, Changchun, China.; Okayama University, JAPAN, |
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| Abstract: | We have screened 11 isoquinoline derivatives and α-methylene-γ-butyrolactones using the 3-(4,5-dimethylthi-azol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay in HeLa and HEK-293T cells. Compound 2 was identified as potential anticancer agent. To further improve its therapeutic potential, this agent was incorporated into transferrin (Tf)-conjugated liposomes (LPs) for targeted delivery to tumor cells. We have demonstrated Tf-LP-Compound 2 have superior antitumor activity compared to non-targeted controls and the free drug. These data show Tf-LP-Compound 2 to be a promising agent that warrants further evaluation. |
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